Discovery of bazedoxifene analogues targeting glycoprotein 130

• Published in: European journal of medicinal chemistry Vol. 199; pp. 112375 - 112393
• Main Authors: Song, Dongmei, Yu, Wenying, Ren, Yuhao, Zhu, Jiawen, Wan, Chengying, Cai, Guiping, Guo, Jianpeng, Zhang, Wenda, Kong, Lingyi
• Format: Journal Article
• Language: English
• Published: ISSY-LES-MOULINEAUX Elsevier Masson SAS 01.08.2020; Elsevier
• Subjects: A549 Cells; Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antitumor activity; Apoptosis - drug effects; Bazedoxifene; Cell Movement - drug effects; Cell Proliferation - drug effects; Cell Survival - drug effects; Chemistry, Medicinal; Cytokine Receptor gp130 - antagonists & inhibitors; Cytokine Receptor gp130 - metabolism; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; GP130; HEK293 Cells; Humans; IL-6; Indoles - chemical synthesis; Indoles - chemistry; Indoles - pharmacology; Life Sciences & Biomedicine; Male; Mice; Mice, Nude; Molecular Docking Simulation; Molecular Structure; Pharmacology & Pharmacy; Science & Technology; STAT3; Structure-Activity Relationship; GP130; Antitumor activity; Bazedoxifene; IL-6; STAT3; COMPLEX; SIGNALING AXIS; SPECIFICITY; CYTOKINE RECEPTOR; GP130 INHIBITOR; IDENTIFICATION

Deregulation of GP130 in signal transduction is involved in multiple types of human diseases, especially in cancers, indicating that GP130 is an attractive target for cancer therapy. However, GP130 was conventionally considered as an undruggable target thus the discovery of GP130 PPI inhibitors is e...